Cytosolic phospholipase A2 (cPLA2), a member of the phospholipase A2 (PLA2) family, releases arachidonic acid from the phospholipid membrane and is the rate-limiting enzyme in the biosynthesis of prostaglandins (PGs), thromboxanes (Txs) and leukotrienes (LTs), all of which are implicated in the body's inflammatory response. Inhibition of this enzyme and other members of the PLA2 family is therefore a potential avenue for the amelioration of inflammatory diseases and conditions (Tibes & Friebe, Phospholipase A2 inhibitors in development. Expert Opin Investig Drugs. 1997 March; 6(3):279-98).
The compound 3-{4-[2-{5-chloro-1-(diphenylmethyl)-2-[2-({[2-(trifluoromethyl)benzyl]sulfonyl}amino)ethyl]-1H-indol-3-yl}ethyl]sulfonyl}phenyl}propanoic acid was identified as part of an effort to identify novel, high-potency inhibitors of cPLA2α (McKew et al. J Med Chem. 2008 Jun. 26; 51(12):3388-413). It may be manufactured as described in WO2006/128142, the contents of which are hereby incorporated by reference.